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Boron Trifluoride Etherate Promoted Microwave-Assisted Synthesis of Antimalarial Acridones.

ABSTRACT: A microwave-assisted, rapid and efficient method using boron trifluoride etherate (BF₃.Et₂O) for the synthesis of acridones, via an intramolecular acylation of N-phenylanthranilic acid derivatives, has been developed. The reaction proceeds under solvent-free conditions, tolerates a wide range of functional groups, and provides rapid access to a range of acridones in good to excellent yields. Several of the synthesized acridones exhibited potent antimalarial activities against CQ sensitive and multi-drug resistant (MDR) parasites.

SUBMITTER: Kancharla P

PROVIDER: S-EPMC8939876 | biostudies-literature | 2019

REPOSITORIES: biostudies-literature

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Boron Trifluoride Etherate Promoted Microwave-Assisted Synthesis of Antimalarial Acridones.

Kancharla Papireddy P Dodean Rozalia A RA Li Yuexin Y Kelly Jane X JX

RSC advances 20191220 72

A microwave-assisted, rapid and efficient method using boron trifluoride etherate (BF3.Et2O) for the synthesis of acridones, via an intramolecular acylation of N-phenylanthranilic acid derivatives, has been developed. The reaction proceeds under solvent-free conditions, tolerates a wide range of functional groups, and provides rapid access to a range of acridones in good to excellent yields. Several of the synthesized acridones exhibited potent antimalarial ac ...[more]

PMID: 35321096

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